Effect of the 5-Hydroxytryptamine_3 (5-HT_3)-Receptor Antagonist KB-R6933 on Experimental Diarrhea Models
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The effects of a 5-hydroxytryptamine<SUB>3</SUB> (5-HT<SUB>3</SUB>)-receptor antagonist KB-R6933 (6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl)-benzimidazole dimaleate) on experimental diarrhea and on intestinal fluid secretion stimulated by cholera toxin were examined and compared with those of ramosetron and loperamide. KB-R6933 and ramosetron (0.03 - 1 mg/kg, p.o.) inhibited the diarrhea induced by 5-HT, but not that by castor oil or prostaglandin E<SUB>2</SUB> (PGE<SUB>2</SUB>), in mice. Loperamide significantly inhibited the diarrhea induced by 5-HT, castor oil and PGE<SUB>2</SUB>. All drugs tested inhibited the diarrhea induced by restraint stress and the intestinal fluid secretion stimulated by cholera toxin in rats. The results suggest the possibility that KB-R6933 may have clinical efficacy in the treatment of diarrhea.
- The Japanese Journal of Pharmacology
The Japanese Journal of Pharmacology 80(1), 93-96, 1999-05-01
The Japanese Pharmacological Society